7-N-Heterocyclyl cephalosporins
AssigneeMerck & Co., Inc.
InventorJohn Hannah
Life of this patent
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Abstract
Disclosed are antibiotic cephalosporins (I) of the formula: ##STR1## Wherein the stylized radical attached to the 7-amino nitrogen of the cephalosporin moiety represents a nitrogen-containing heterocyclic group (mono- or polycyclic); R is, inter alia, hydrogen, alkyl, heterocyclylalkyl, aryl, alkenyl, aralkyl, --NR.sub.2, --OR, COOR, CONR.sub.2 or CN; A is conventionally known in the cephalosporin art; and R.sup.2 is H, or lower alkoxyl. Also disclosed are the pharmaceutically acceptable salt and ester derivatives of I; processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
Claims5
A compound having the structural formula:
- ##STR322## and the pharmaceutically acceptable salts thereof wherein:
- R.sup.2 is hydrogen or methoxyl;
- R' is selected from the group consisting of:
- ##STR323## wherein the dotted line indicates both saturated and unsaturated rings;
- and wherein:
- A is selected from the group consisting of:
- ##STR324## wherein Y is a pharmaceutically acceptable anion and M is a pharmaceutically acceptable cation;
- R is hydrogen, alkyl having from 1-6 carbon atoms, substituted alkyl having from 1-6 carbon atoms wherein the substituent is chloro, fluoro, hydroxyl, alkoxyl (C.sub.1-6), carboxyl, amino, sulfo and mono- and dialkylamino wherein each alkyl has 1-6 carbon atoms substituted and unsubstituted phenylalkyl and phenylalkenyl having 7-12 carbon atoms wherein the substituent is selected from chloro, fluoro, carboxyl, amino, cyano, hydroxyl and sulfo;
- R.sup.3 is chloro, fluoro, hydroxyl, carboxyl, sulfo, cyano, amino, mono- and dialkylamino, alkoxyl, alkyl having from 1-6 carbon atoms, substituted alkyl having 1-6 carbon atoms wherein the substituent is carboxyl, cyano, alkoxyl having 1-6 carbon atoms, phenyl and phenyloxy;
- and
- n is an integer selected from 0 to 3.
The compound 4-[{3-[{(1-methyltetrazol-5-yl)thio}methyl]-2-carboxy-8-oxo-5-thia-1-azabi cyclo[4.2.0]oct-2-en-7.beta.-yl}amino]-1-benzylpyridinium hydroxide inner salt having the structure:
- ##STR327## and the pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.